Derivatives of tamoxifen. Dependence of antiestrogenicity on the 4-substituent

R McCague, G Leclercq, N Legros…

Index: McCague, Raymond; Leclercq, Guy; Legros, Nicole; Goodman, Joyce; Blackburn, G. Michael; et al. Journal of Medicinal Chemistry, 1989 , vol. 32, # 12 p. 2527 - 2533

Full Text: HTML

Citation Number: 85

Abstract

A range of tamoxifen derivatives substituted in the 4-position of the 1-phenyl ring are described. The key steps in the synthesis of I-iOdO-, 4-bromo-, and 4-(methy1thio) tamoxifen were reactions of 1, 2-diarylbutanones with the (4-halogenopheny1) lithium or [4- (methy1thio) phenyllmagnesium bromide. Oxidized precursors of 4-(methylthio) tamoxifen were used to prepare the methylsulfinyl and methylsulfonyl derivatives. Further derivatives ...